Toxicity, mammalian

The field of organogermanium chemistry is becoming increasingly important. Gertain germanium compounds have a low mammalian toxicity, but a marked activity against certain bacteria, which makes them useful as chemotherapeutic agents. 

Pyrethroids from Chiysanthemic Acid. The unsaturated side chains of the aHethrolone alcohol moieties of the natural pyrethrins are readily epoxidized by microsomal oxidases and converted to diols, thus detoxifying the insecticides. Esterification of chrysanthemic acid (9), R = CH3, with substituted ben2yl alcohols produces usehil insecticides barthrin [70-43-9J, 2-chloro-3,4-methylenedioxyben2yl (+)-i7j ,/n7 j -chrysanthemate, and dimethrin [70-38-2] 2,4-dimethylben2yl (+)-i7j ,/n7 j -chrysanthemate. These have alimited spectmm of insecticidal activity but are of very low mammalian toxicity, ie, rat oralLD s >20,000 mg/kg. 

Perthane [72-56-0] l,l-dichloro-2,2-bis-(4-ethyiphenyi)ethane (30) (mp 60—61°C) is a rapidly biodegradable insecticide with very low mammalian toxicity, rat oral LD q 8170 mg/kg. It has been used as a household insecticide. 

Insect Growth Regulators. These compounds (40—45), unlike most conventional insecticides, interfere with biochemical processes that are unique to arthropods eg, molting, ecdysis, and formation of the chitinous exoskeleton. Therefore, they are selective insecticides with very low mammalian toxicity. 

The mode of action of the naphthoquinoid ansamacroHdes was estabHshed through studies using the tifamycins and streptovaricins (84,141,257,258). The ansamacroHdes inhibit bacterial growth by inhibiting RNA synthesis. This is accompHshed by forming a tight complex with DNA-dependent RNA polymerase. This complex is between the ansamacroHde and the P-unit of RNA polymerase. The formation of the complex inhibits the initation step of RNA synthesis (259,260). The ansamacroHdes form no such complex with mammalian RNA polymerase and thus have low mammalian toxicity. 

The mechanism of antibacterial activity is through inhibition of gram-positive bacterial cell-wall synthesis thus, the penicillins are most effective against actively multiplying organisms. Because mammalian cells do not have a definitive cell-wall stmcture as do bacteria, the mammalian toxicity of the penicillins is low. Allergic phenomena in patients following sensitization may occur. 

In 1962, bromacil (5-bromo-3-s-butyl-6-methyluracil 1047 R = Bu ), its homologue (isocil 1047 R = Pr ) and related iV-alkyluracils were shown to have valuable selective phytotoxic properties and vitually no mammalian toxicity. Thus, bromacil achieves a complete kill of most unwanted broad-leaf annuals or perennials along with some grasses... 

It is obvious from the provisional risk assessment values for microcystins, and, being of the same order of magnitude of mammalian toxicity, similar values may be calculated for the cyanobacterial neurotoxins, that sensitive detection methods are required to detect these low concentrations of toxins. Of the biological methods of detection discussed earlier, the mouse and invertebrate bioassays are not sensitive enough without concentration of water samples, in that they are only able to detect mg of microcystins per litre. Only the immunoassays (ng-/rg 1 and the protein phosphatase inhibition assays (ng O... 

NOTE Glycol selection should also take into account the risk of leaks to the environment and the ultimate safe disposal of the material. Propylene glycol is a safer alternative to ethylene glycol because of its very low mammalian toxicity. 

Ascher and Nemny 495) found that residues of triphenyltin acetate on glass, resulting from the evaporation of acetone solutions thereof, were, on contact to houseflies, less toxic with rising concentration. As triphenyltin acetate is likely to be a self-associated polymer in the solid state [similar to trimethyltin acetate (355)] and in concentrated solutions, it was suggested 495) that the monomer, which exists in dilute solutions, is toxic to insects, and the polymer, nontoxic. Interestingly, in this connection, a triphenyltin methacrylate copolymer has 470) a very low mammalian toxicity (acute, oral LDso for mice >2000 mg/kg). 

It may, therefore, be seen that the mammalian toxicity of the lower dialkyltin compounds, unlike that of their trialkyltin counterparts, is markedly dependent upon the nature of the X groups this is probably true for species other than mammals (e.g., fungi) if the mode of action is similar. 

Herbicides constitute a large and diverse class of pesticides that, with a few exceptions, have very low mammalian toxicity and have received relatively little attention as environmental pollutants. Much of the work in the held of ecotoxicology and much environmental risk assessment has focused on animals, especially vertebrate animals. There has perhaps been a tendency to overlook the importance of plants in the natural world. Most plants belong to the lowest trophic levels of ecosystems, and animals in higher trophic levels are absolutely dependent on them for their survival. 

PCP presents a different picture from that of the lower chlorophenols and their derivatives. The corresponding dioxin shows much more stability to light than does TCDD, enough to permit its prolonged existence at low concentrations in a photoreactor. As a phenol it can directly yield dioxins, a process favored by its normal mode of application as the sodium salt. Although octachlorodibenzo-p-dioxin has much lower mammalian toxicity than TCDD (6), its formation, properties, and effects demand additional investigation. Technical preparations of PCP are frequently mixtures of tetra- and pentachlorophenols consequently, hepta-and possibly hexachlorodibenzo-p-dioxins might be expected as photolysis products in addition to the octachloro derivative. 

Devillers J. Prediction of mammalian toxicity of organophosphorns pesticides from QSTR modeling. SAR QSAR Environ Res 2004 15 501-10. 

Substances with very high acute mammalian toxicity Substances with very high acute or chronic aquatic toxicity Neurotoxins... 

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